Enobosarm
drugOn this page
Also known as GTX-024MK-2866OstarineSID174007253MK-2866 (GTX-024)
Summary
Enobosarm (CHEMBL1738889) is a phase-3 clinical-stage small molecule; indicated across 6 conditions including non-small cell lung carcinoma and muscular atrophy.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Indications: 6 conditions
- Clinical trials: 16
- Chemistry: 389.3 Da · C19H14F3N3O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1738889 |
| Name | Enobosarm |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 11326715 |
| Molecular formula | C19H14F3N3O3 |
| Molecular weight | 389.3 |
| InChIKey | JNGVJMBLXIUVRD-SFHVURJKSA-N |
SMILES: C[C@](COC1=CC=C(C=C1)C#N)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O
IUPAC name: (2S)-3-(4-cyanophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide
Also known as: Enobosarm, GTX-024, Gtx-024, MK-2866, Ostarine, ENOBOSARM, ostarine, SID174007253, MK-2866 (GTX-024), MK-2866 (GTx-024)
Patent coverage: 269 distinct patent families (756 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 701 (93%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Androgen receptor, Androgen receptor.
Bioactivity
ChEMBL activities: 11 potent at pChembl ≥ 5 of 11 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| AR | 9.26 | Ki | 0.55 | nM | CHEMBL_ACT_24824181 |
| AR | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_25528490 |
| AR | 8.42 | IC50 | 3.8 | nM | CHEMBL_ACT_19293360 |
| AR | 8.42 | Ki | 3.8 | nM | CHEMBL_ACT_19293401 |
| AR | 7.7 | Ki | 20.2 | nM | CHEMBL_ACT_28149125 |
| AR | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_28149128 |
| AR | 7.7 | Ki | 20.2 | nM | CHEMBL_ACT_28598786 |
| AR | 7.7 | Ki | 20.2 | nM | CHEMBL_ACT_28995968 |
| AR | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_28995971 |
| P15207 | 7.44 | IC50 | 36.4 | nM | CHEMBL_ACT_19467342 |
| AR | 7.42 | Ki | 38 | nM | CHEMBL_ACT_25528543 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
6 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| non-small cell lung carcinoma | 3 | MONDO:0005233 | EFO:0003060 |
| muscular atrophy | 3 | MONDO:0004323 | EFO:0009851 |
| breast neoplasm | 3 | MONDO:0021100 | MONDO:0007254 |
| triple-negative breast carcinoma | 2 | MONDO:0005494 | EFO:0005537 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 16.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 11 |
| PHASE3 | 4 |
| PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01355484 | PHASE3 | COMPLETED | Phase III Study of the Effect of GTx-024 on Muscle Wasting in Patients With Non-Small Cell Lung Cancer (NSCLC) |
| NCT01355497 | PHASE3 | COMPLETED | Effect of GTx-024 on Muscle Wasting in Patients With Non-Small Cell Lung Cancer (NSCLC) on First Line Platinum |
| NCT04869943 | PHASE3 | TERMINATED | Efficacy Evaluation of Enobosarm Monotherapy in Treatment of AR+/ER+/HER2- Metastatic Breast Cancer |
| NCT05065411 | PHASE3 | TERMINATED | Efficacy & Safety Evaluation of Enobosarm in Combo With Abemaciclib in Treatment of ER+HER2- Metastatic Breast Cancer |
| NCT07446998 | PHASE2 | RECRUITING | Proof-of-Concept Study Evaluating Total Body Weight, Physical Function & Safety of Enobosarm in Patients Treated With GLP-1 Receptor Agonist, for Weight Loss |
| NCT00467844 | PHASE2 | COMPLETED | Study of GTx-024 on Muscle Wasting (Cachexia) Cancer. |
| NCT01616758 | PHASE2 | TERMINATED | Phase II Study of GTx024 in Women With Metastatic Breast Cancer |
| NCT02368691 | PHASE2 | TERMINATED | Efficacy and Safety of GTx-024 in Patients With Androgen Receptor-Positive Triple Negative Breast Cancer (AR+ TNBC) |
| NCT02463032 | PHASE2 | COMPLETED | Efficacy and Safety of GTx-024 in Patients With Estrogen Receptor (ER)+/Androgen Receptor (AR)+ Breast Cancer |
| NCT02658448 | PHASE2 | COMPLETED | GTx-024 as a Treatment for Stress Urinary Incontinence in Women |
| NCT02746328 | PHASE2 | WITHDRAWN | Add-on Study for Protocol G200802 (NCT02463032): Effect of GTx-024 on Maximal Neuromuscular Function and Lean Body Mass |
| NCT02971761 | PHASE2 | COMPLETED | Pembrolizumab and Enobosarm in Treating Patients With Androgen Receptor Positive Metastatic Triple Negative Breast Cancer |
| NCT03508648 | PHASE2 | WITHDRAWN | Durability Extension Study to Assess Clinical Activity and Safety of Enobosarm (GTx-024) in Stress Urinary Incontinence |
| NCT03566290 | PHASE2 | WITHDRAWN | Study to Assess Long-Term Safety/Tolerability of Enobosarm (GTx 024) in Stress Urinary Incontinence |
| NCT06282458 | PHASE2 | COMPLETED | Dose-Finding Study Evaluating Effect on Body Composition of Enobosarm in Patients Taking a GLP-1 for Chronic Weight Mgmt |
| NCT03264651 | PHASE1 | COMPLETED | Enobosarm and Anastrozole in Pre-menopausal Women With High Mammographic Breast Density |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).